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Page 1
Discovery and characterization of orally bioavailable 4-chloro-6-fluoroisophthalamides as covalent PPARG inverse-agonists.
Orsi DL, Ferrara SJ, Siegel S, Friberg A, Bouché L, Pook E, Lienau P, Bluck JP, Lemke CT, Akcay G, Stellfeld T, Meyer H, Pütter V, Holton SJ, Korr D, Jerchel-Furau I, Pantelidou C, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: putter v. Bioorg Med Chem. 2023 Jan 15;78:117130. doi: 10.1016/j.bmc.2022.117130. Epub 2022 Dec 13. Bioorg Med Chem. 2023. PMID: 36542958 Free article.
Correction to "Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069".
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: putter v. J Med Chem. 2023 Jan 12;66(1):1082. doi: 10.1021/acs.jmedchem.2c02002. Epub 2022 Dec 21. J Med Chem. 2023. PMID: 36542814 Free PMC article. No abstract available.
CACHE Challenge #1: Targeting the WDR Domain of LRRK2, A Parkinson's Disease Associated Protein.
Li F, Ackloo S, Arrowsmith CH, Ban F, Barden CJ, Beck H, Beránek J, Berenger F, Bolotokova A, Bret G, Breznik M, Carosati E, Chau I, Chen Y, Cherkasov A, Corte DD, Denzinger K, Dong A, Draga S, Dunn I, Edfeldt K, Edwards A, Eguida M, Eisenhuth P, Friedrich L, Fuerll A, Gardiner SS, Gentile F, Ghiabi P, Gibson E, Glavatskikh M, Gorgulla C, Guenther J, Gunnarsson A, Gusev F, Gutkin E, Halabelian L, Harding RJ, Hillisch A, Hoffer L, Hogner A, Houliston S, Irwin JJ, Isayev O, Ivanova A, Jacquemard C, Jarrett AJ, Jensen JH, Kireev D, Kleber J, Koby SB, Koes D, Kumar A, Kurnikova MG, Kutlushina A, Lessel U, Liessmann F, Liu S, Lu W, Meiler J, Mettu A, Minibaeva G, Moretti R, Morris CJ, Narangoda C, Noonan T, Obendorf L, Pach S, Pandit A, Perveen S, Poda G, Polishchuk P, Puls K, Pütter V, Rognan D, Roskams-Edris D, Schindler C, Sindt F, Spiwok V, Steinmann C, Stevens RL, Talagayev V, Tingey D, Vu O, Walters WP, Wang X, Wang Z, Wolber G, Wolf CA, Wortmann L, Zeng H, Zepeda CA, Zhang KYJ, Zhang J, Zheng S, Schapira M. Li F, et al. Among authors: putter v. J Chem Inf Model. 2024 Nov 25;64(22):8521-8536. doi: 10.1021/acs.jcim.4c01267. Epub 2024 Nov 5. J Chem Inf Model. 2024. PMID: 39499532
Dual targeting of the androgen receptor and PI3K/AKT/mTOR pathways in prostate cancer models improves antitumor efficacy and promotes cell apoptosis.
Sugawara T, Nevedomskaya E, Heller S, Böhme A, Lesche R, von Ahsen O, Grünewald S, Nguyen HM, Corey E, Baumgart SJ, Georgi V, Pütter V, Fernández-Montalván A, Vasta JD, Robers MB, Politz O, Mumberg D, Haendler B. Sugawara T, et al. Among authors: putter v. Mol Oncol. 2024 Mar;18(3):726-742. doi: 10.1002/1878-0261.13577. Epub 2024 Jan 15. Mol Oncol. 2024. PMID: 38225213 Free PMC article.
Discovery and Structure-Based Design of Potent Covalent PPARγ Inverse-Agonists BAY-4931 and BAY-0069.
Orsi DL, Pook E, Bräuer N, Friberg A, Lienau P, Lemke CT, Stellfeld T, Brüggemeier U, Pütter V, Meyer H, Baco M, Tang S, Cherniack AD, Westlake L, Bender SA, Kocak M, Strathdee CA, Meyerson M, Eis K, Goldstein JT. Orsi DL, et al. Among authors: putter v. J Med Chem. 2022 Nov 10;65(21):14843-14863. doi: 10.1021/acs.jmedchem.2c01379. Epub 2022 Oct 21. J Med Chem. 2022. PMID: 36270630 Free PMC article.
Discovery and Characterization of the Potent and Highly Selective 1,7-Naphthyridine-Based Inhibitors BAY-091 and BAY-297 of the Kinase PIP4K2A.
Wortmann L, Bräuer N, Holton SJ, Irlbacher H, Weiske J, Lechner C, Meier R, Karén J, Siöberg CB, Pütter V, Christ CD, Ter Laak A, Lienau P, Lesche R, Nicke B, Cheung SH, Bauser M, Haegebarth A, von Nussbaum F, Mumberg D, Lemos C. Wortmann L, et al. Among authors: putter v. J Med Chem. 2021 Nov 11;64(21):15883-15911. doi: 10.1021/acs.jmedchem.1c01245. Epub 2021 Oct 26. J Med Chem. 2021. PMID: 34699202 Free article.
The RESOLUTE consortium: unlocking SLC transporters for drug discovery.
Superti-Furga G, Lackner D, Wiedmer T, Ingles-Prieto A, Barbosa B, Girardi E, Goldmann U, Gürtl B, Klavins K, Klimek C, Lindinger S, Liñeiro-Retes E, Müller AC, Onstein S, Redinger G, Reil D, Sedlyarov V, Wolf G, Crawford M, Everley R, Hepworth D, Liu S, Noell S, Piotrowski M, Stanton R, Zhang H, Corallino S, Faedo A, Insidioso M, Maresca G, Redaelli L, Sassone F, Scarabottolo L, Stucchi M, Tarroni P, Tremolada S, Batoulis H, Becker A, Bender E, Chang YN, Ehrmann A, Müller-Fahrnow A, Pütter V, Zindel D, Hamilton B, Lenter M, Santacruz D, Viollet C, Whitehurst C, Johnsson K, Leippe P, Baumgarten B, Chang L, Ibig Y, Pfeifer M, Reinhardt J, Schönbett J, Selzer P, Seuwen K, Bettembourg C, Biton B, Czech J, de Foucauld H, Didier M, Licher T, Mikol V, Pommereau A, Puech F, Yaligara V, Edwards A, Bongers BJ, Heitman LH, IJzerman AP, Sijben HJ, van Westen GJP, Grixti J, Kell DB, Mughal F, Swainston N, Wright-Muelas M, Bohstedt T, Burgess-Brown N, Carpenter L, Dürr K, Hansen J, Scacioc A, Banci G, Colas C, Digles D, Ecker G, Füzi B, Gamsjäger V, Grandits M, Martini R, Troger F, Altermatt P, Doucerain C, Dürrenberger F, Manolova V, Steck AL, Sundström H, Wilhelm M, Steppan CM. Superti-Furga G, et al. Among authors: putter v. Nat Rev Drug Discov. 2020 Jul;19(7):429-430. doi: 10.1038/d41573-020-00056-6. Nat Rev Drug Discov. 2020. PMID: 32265506 No abstract available.
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